Anticancer agents with tumor selectivity are the holy grail of cancer research.  The present study focuses on combining peptidic ligands with boron-containing entities to afford novel conjugates for use in Boron Neutron Capture Therapy (BNCT).  In BNCT, ¹⁰B-containing agents are delivered to tumor cells and undergo rapid fission upon irradiation with neutrons to produce energetic ⁷Li³⁺ and ⁴He²⁺.¹  To maximise cell destruction, the compound must exhibit tumor selectivity.¹  This requirement may be addressed by using cyclic RGD peptides which bind to integrin receptors that are over-expressed on tumor cells,² and hence have the potential to deliver boron selectively to tumour cells.  We are synthesizing a series of compounds (1 - 6) consisting of a cyclic RGD peptide and boron moiety.  Key results will be presented. 

References

[1] Soloway, A. H. et al, Chem. Rev. 1998,  98,  1515-1562.  [2] Haubner, R. et al, H. J. Am. Chem. Soc. 1996, 118, 7461-7472.